Assay Detail
Binding
CHEMBL5133801
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Inhibition of pBTK in human whole blood
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.21 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200748 | — | — | 1 | 6.92 |
| CHEMBL5170218 | — | — | 1 | 6.51 |
| CHEMBL5192675 | — | — | 1 | 6.46 |
| CHEMBL5192152 | — | — | 1 | 6.32 |
| CHEMBL5169775 | — | — | 1 | 6.23 |
| CHEMBL5189116 | — | — | 1 | 6.09 |
| CHEMBL5204655 | — | — | 1 | 6.03 |
| CHEMBL5170919 | — | — | 1 | 6.00 |
| CHEMBL5188545 | — | — | 1 | 5.98 |
| CHEMBL5208570 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200748 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5170218 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5192675 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5192152 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5169775 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5189116 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5204655 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL5170919 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL5188545 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5208570 | — | IC50 | = | 2650.0 | nM | 5.58 |